2. Academic Validation
  3. Cytotoxic simplified tubulysin analogues

Cytotoxic simplified tubulysin analogues

  • J Med Chem. 2008 Mar 27;51(6):1530-3. doi: 10.1021/jm701321p.
Bhooma Raghavan 1,  Ranganathan Balasubramanian,  Jaeson C Steele,  Dan L Sackett,  Robert A Fecik
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry. 308 Harvard Street SE, University of Minnesota, Minneapolis, MN 55455, USA.
PMID: 18314944 DOI: 10.1021/jm701321p
Abstract

An efficient route for the synthesis of the tubulysin family of antimitotic peptides was developed. Simplified tubulysin analogues were synthesized to define the minimum pharmacophore required for cytotoxicity. Simplified tubulysin analogues retain significant cytotoxicity and reveal important preliminary structure-activity relationships.

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